Structural insights into G-protein-coupled receptor activation.
G-protein-coupled receptors (GPCRs) are the largest family of eukaryotic plasma membrane receptors, and are responsible for the majority of cellular responses to external signals. GPCRs share a common architecture comprising seven transmembrane (TM) helices. Binding of an activating ligand enables the receptor to catalyze the exchange of GTP for GDP in a heterotrimeric G protein. GPCRs are in a conformational equilibrium between inactive and activating states. Crystallographic and spectroscopic studies of the visual pigment rhodopsin and two beta-adrenergic receptors have defined some of the conformational changes associated with activation.
Weis
William I
WI
Department of Molecular & Cellular Physiology, Stanford University School of Medicine, USA. bill.weis@stanford.edu
Kobilka
Brian K
BK
D000818:Animals; D003461:Crystallography; D006801:Humans; D008565:Membrane Proteins / Q000737:chemistry / Q000378:metabolism; D008958:Models, Molecular; D011943:Receptors, Adrenergic, beta / Q000737:chemistry / Q000378:metabolism; D043562:Receptors, G-Protein-Coupled / Q000737:chemistry* / Q000378:metabolism*; D012243:Rhodopsin / Q000737:chemistry / Q000378:metabolism
D008565:Membrane Proteins; D011943:Receptors, Adrenergic, beta; D043562:Receptors, G-Protein-Coupled; D012243:Rhodopsin